Apabetalone (RVX-208): A Potential Epigenetic Therapy for the Treatment of Cardiovascular, Renal, Neurological, Viral, and Cancer Disorders
Author | Dhulkifle, Hevna |
Author | Diab, Mohammad Issam |
Author | Algonaiah, Majed |
Author | Korashy, Hesham M. |
Author | Maayah, Zaid H. |
Available date | 2024-04-29T11:04:12Z |
Publication Date | 2024-02-06 |
Publication Name | ACS Pharmacology and Translational Science |
Identifier | http://dx.doi.org/10.1021/acsptsci.3c00219 |
Citation | Dhulkifle, H., Diab, M. I., Algonaiah, M., Korashy, H. M., & Maayah, Z. H. (2024). Apabetalone (RVX-208): A Potential Epigenetic Therapy for the Treatment of Cardiovascular, Renal, Neurological, Viral, and Cancer Disorders. ACS Pharmacology & Translational Science, 7(3), 546-559. |
Abstract | Bromodomain and extra-terminal domain proteins (BET proteins) are epigenetic reader proteins that have been implicated in regulating gene expression through binding to chromatin and interaction with transcription factors. These proteins are located in the nucleus and are responsible for recognizing acetylated lysine residues on histones, reading epigenetic messages, recruiting key transcription factors, and thereby regulating gene expression. BET proteins control the transcription of genes responsible for maladaptive effects in inflammation, cancer, and renal and cardiovascular diseases. Given the multifaceted role of BET proteins in the pathogenesis of various diseases, several small molecule inhibitors of BET proteins have been developed as potential therapeutic targets for treating different diseases in recent years. However, while many nonselective BET inhibitors are indicated for the treatment of cancer, a selective BET inhibitor, apabetalone, is the only oral BET inhibitor in phase III clinical trials for the treatment of cardiovascular diseases and others. Thus, this review aims to present and discuss the preclinical and clinical evidence for the beneficial effects and mechanism of action of apabetalone for treating various diseases. |
Sponsor | This publication was supported by Qatar University Internal Grant No. QUCG-CPH-23/24-209. |
Language | en |
Publisher | American Chemical Society (ACS) |
Subject | Apabetalone cardiovascular epigenetics inflammation |
Type | Article |
Pagination | 546-559 |
Issue Number | 3 |
Volume Number | 7 |
ESSN | 2575-9108 |
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